Fludeoxyglucose (18F)
Identification
- Summary
Fludeoxyglucose (18F) is a radiopharmaceutical agent used for positron emission tomography (PET) imaging in oncology, cardiology, and neurology.
- Generic Name
- Fludeoxyglucose (18F)
- DrugBank Accession Number
- DB09502
- Background
Fludeoxyglucose F 18 Injection is a positron emitting radiopharmaceutical containing no-carrier added radioactive 2-deoxy-2-[18F]fluoro-D-g1ucose, which is used for diagnostic purposes in conjunction with Positron Emission Tomography (PET). It is administered by intravenous injection.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 181.15
Monoisotopic: 181.061586121 - Chemical Formula
- C6H11FO5
- Synonyms
- (18F)-FDG
- 18-F FDG
- 18F-FDG
- Fludeoxyglucose (18F)
- Fludeoxyglucose F 18
- Fludeoxyglucose F-18
- Fludeoxyglucose, F-18
- Fluorine (18F) fludeoxyglucose
Pharmacology
- Indication
The uptake of 18F-FDG by tissues is a marker for the tissue uptake of glucose, which in turn is closely correlated with certain types of tissue metabolism. Fludeoxyglucose F 18 Injection is indicated in positron emission tomography (PET) imaging for assessment of abnormal glucose metabolism to assist in the evaluation of malignancy in patients with known or suspected abnormalities found by other testing modalities, or in patients with an existing diagnoses of cancer.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Diagnostic agent Cancer •••••••••••• Diagnostic agent Coronary artery disease •••••••••••• Diagnostic agent Epileptic seizure •••••••••••• Diagnostic agent Left ventricular dysfunction •••••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Fludeoxyglucose F 18 Injection is rapidly distributed to all organs of the body after intravenous administration. After background clearance of Fludeoxyglucose F 18 Injection, optimal PET imaging is generally achieved between 30 to 40 minutes after administration. In cancer, the cells are generally characterized by enhanced glucose metabolism partially due to (1) an increase in the activity of glucose transporters, (2) an increased rate of phosphorylation activity, (3) a reduction of phosphatase activity or, (4) a dynamic alteration in the balance among all these processes. However, glucose metabolism of cancer as reflected by Fludeoxyglucose F 18 accumulation shows considerable variability. Depending on tumor type, stage, and location, Fludeoxyglucose F 18 accumulation may be increased, normal, or decreased. Also, inflammatory cells can have the same variability of uptake of Fludeoxyglucose F 18. In the heart, under normal aerobic conditions, the myocardium meets the bulk of its energy requirements by oxidizing free fatty acids. Most of the exogenous glucose taken up by the myocyte is converted into glycogen. However, under ischemic conditions, the oxidation of free fatty acids decreases, exogenous glucose becomes the preferred myocardial substrate, glycolysis is stimulated, and glucose taken up by the myocyte is metabolized immediately instead of being converted into glycogen. Under these conditions, phosphorylated Fludeoxyglucose F 18 accumulates in the myocyte and can be detected with PET imaging. Normally, the brain relies on anaerobic metabolism. In epilepsy, the glucose metabolism varies. Generally, during a seizure glucose metabolism increases. Interictally, the seizure focus tends to be hypometabolic.
- Mechanism of action
Fludeoxyglucose F 18 is a glucose analog that concentrates in cells that rely upon glucose as an energy source, or in cells whose dependence on glucose increases under pathophysiological conditions. Fludeoxyglucose F 18 is transported through the cell membrane by facilitative glucose transporter proteins and is phosphorylated within the cell to [18F] FDG-6- phosphate by the enzyme hexokinase. Once phosphorylated it cannot exit until it is dephosphorylated by glucose-6-phosphatase. Therefore, within a given tissue or pathophysiological process, the retention and clearance of Fludeoxyglucose F 18 reflect a balance involving glucose transporter, hexokinase and glucose-6- phosphatase activities. When allowance is made for the kinetic differences between glucose and Fludeoxyglucose F 18 transport and phosphorylation (expressed as the “lumped constant” ratio), Fludeoxyglucose F 18 is used to assess glucose metabolism. In comparison to background activity of the specific organ or tissue type, regions of decreased or absent uptake of Fludeoxyglucose F 18 reflect the decrease or absence of glucose metabolism. Regions of increased uptake of Fludeoxyglucose F 18 reflect greater than normal rates of glucose metabolism.
- Absorption
Fludeoxyglucose F 18 Injection is rapidly distributed to all organs of the body after intravenous administration.
- Volume of distribution
Fludeoxyglucose F 18 Injection is rapidly distributed to all organs of the body after intravenous administration.
- Protein binding
The extent of binding of Fludeoxyglucose F 18 to plasma proteins is not known.
- Metabolism
Fludeoxyglucose F 18 is transported into cells and phosphorylated to [18F]-FDG-6-phosphate at a rate proportional to the rate of glucose utilization within that tissue. [18F]-FDG-6-phosphate presumably is metabolized to 2-deoxy-2-[18F] fluoro-6-phospho-Dmannose ([18F]FDM-6-phosphate). Fludeoxyglucose F 18 Injection may contain several impurities (e.g., 2-deoxy-2-chloro-D-glucose (ClDG)). Biodistribution and metabolism of C1DG are presumed to be similar to Fludeoxyglucose F 18 and would be expected to result in intracellular formation of 2-deoxy-2-chloro-6-phospho-D-glucose (C1DG-6-phosphate) and 2-deoxy-2-chloro-6-phospho-D-mannose (ClDM-6-phosphate). The phosphorylated deoxyglucose compounds are dephosphorylated and the resulting compounds (FDG, FDM, C1DG, and ClDM) presumably leave cells by passive diffusion.
- Route of elimination
Fludeoxyglucose F 18 is cleared from most tissues within 24 hours and can be eliminated from the body unchanged in the urine.
- Half-life
10-13 minutes
- Clearance
Fludeoxyglucose F 18 and related compounds are cleared from non-cardiac tissues within 3 to 24 hours after administration. Clearance from the cardiac tissue may require more than 96 hours
- Adverse Effects
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- Toxicity
Overdoses of Fludeoxyglucose F 18 Injection have not been reported.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Fludeoxyglucose (18F) which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Fludeoxyglucose (18F) which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Fludeoxyglucose (18F) which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Fludeoxyglucose (18F) which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Fludeoxyglucose (18F) which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- Take on an empty stomach. When using Fludeoxyglucose (18F) in oncology or neurology, avoid eating for 4-6 hours before Fludeoxyglucose (18F) administration.
- Take with food. Consuming food or beverages containing 50-75 grams of glucose just before the administration of Fludeoxyglucose (18F) may be beneficial in the setting of cardiology imaging.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fludeoxyglucose F 18 Injection, solution 475 mCi/1mL Intravenous Triad Isotopes, Inc. 2010-11-20 2010-11-20 US Fludeoxyglucose F18 Injection 300 mCi/1mL Intravenous Feinstein Institute For Medical Research 2005-08-19 Not applicable US Fludeoxyglucose F18 Injection 400 mCi/1mL Intravenous THE FEINSTEIN INSTITUTE FOR MEDICAL RESEARCH 2005-08-19 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fludeoxyglucose F 18 Injection 500 mCi/1mL Intravenous Hot Shots Nm, Llc Dba Midwest Positron Technology, Lc 2014-08-24 Not applicable US Fludeoxyglucose F 18 Injection 20 mCi/1mL Intravenous Global Isotopes, Llc D/B/A Zevacor Molecular 2014-10-31 2019-05-17 US Fludeoxyglucose F 18 Injection 40 mCi/1mL Intravenous University Of California, Los Angeles 2013-06-27 Not applicable US Fludeoxyglucose F 18 Injection 40 mCi/1mL Intravenous Kettering Medical Center 2011-12-08 Not applicable US Fludeoxyglucose F 18 Injection 20 mCi/1mL Intravenous Decatur Memorial Hospital 2019-11-06 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Fludeoxyglucose F 18 Fludeoxyglucose (18F) (475 mCi/1mL) Injection, solution Intravenous Triad Isotopes, Inc. 2010-11-20 2010-11-20 US
Categories
- ATC Codes
- V09IX04 — Fludeoxyglucose (18f)
- Drug Categories
- Carbohydrates
- Compounds used in a research, industrial, or household setting
- Deoxy Sugars
- Deoxyglucose
- Diagnostic Radiopharmaceuticals
- Diagnostic Uses of Chemicals
- Drugs that are Mainly Renally Excreted
- Indicators and Reagents
- Laboratory Chemicals
- Radioactive Diagnostic Agent
- Radiopharmaceutical Activity
- Radiopharmaceuticals
- Tumour Detection
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as beta-hydroxy aldehydes. These are organic compounds containing an aldehyde substituted with a hydroxy group on the second carbon atom.
- Kingdom
- Organic compounds
- Super Class
- Organic oxygen compounds
- Class
- Organooxygen compounds
- Sub Class
- Carbonyl compounds
- Direct Parent
- Beta-hydroxy aldehydes
- Alternative Parents
- Secondary alcohols / Fluorohydrins / Polyols / Primary alcohols / Organofluorides / Organic oxides / Hydrocarbon derivatives / Alkyl fluorides
- Substituents
- Alcohol / Aliphatic acyclic compound / Alkyl fluoride / Alkyl halide / Beta-hydroxy aldehyde / Fluorohydrin / Halohydrin / Hydrocarbon derivative / Organic oxide / Organofluoride
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- 2-deoxy-2-fluoro-aldehydo-D-glucose, 2-deoxy-2-((18)F)fluoro-D-glucose (CHEBI:49136)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 0Z5B2CJX4D
- CAS number
- 63503-12-8
- InChI Key
- AOYNUTHNTBLRMT-MXWOLSILSA-N
- InChI
- InChI=1S/C6H11FO5/c7-3(1-8)5(11)6(12)4(10)2-9/h1,3-6,9-12H,2H2/t3-,4+,5+,6+/m0/s1/i7-1
- IUPAC Name
- (2R,3S,4R,5R)-2-(¹⁸F)fluoro-3,4,5,6-tetrahydroxyhexanal
- SMILES
- [H]C(=O)[C@H]([18F])[C@@H](O)[C@H](O)[C@H](O)CO
References
- General References
- Tragardh M, Moller N, Sorensen M: Methodologic Considerations for Quantitative 18F-FDG PET/CT Studies of Hepatic Glucose Metabolism in Healthy Subjects. J Nucl Med. 2015 Sep;56(9):1366-71. doi: 10.2967/jnumed.115.154211. Epub 2015 Jul 9. [Article]
- Mega MS, Dinov ID, Porter V, Chow G, Reback E, Davoodi P, O'Connor SM, Carter MF, Amezcua H, Cummings JL: Metabolic patterns associated with the clinical response to galantamine therapy: a fludeoxyglucose f 18 positron emission tomographic study. Arch Neurol. 2005 May;62(5):721-8. [Article]
- Perani D, Bressi S, Testa D, Grassi F, Cortelli P, Gentrini S, Savoiardo M, Caraceni T, Fazio F: Clinical/metabolic correlations in multiple system atrophy. A fludeoxyglucose F 18 positron emission tomographic study. Arch Neurol. 1995 Feb;52(2):179-85. [Article]
- FDA Label [Link]
- External Links
- PubChem Compound
- 68614
- PubChem Substance
- 347827867
- ChemSpider
- 61878
- 1362737
- ChEBI
- 49136
- ChEMBL
- CHEMBL1808698
- ZINC
- ZINC000100079041
- Wikipedia
- Fluorodeoxyglucose_(18F)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Enrolling by Invitation Diagnostic Brain Imaging / Whole Body Imaging 1 4 Recruiting Diagnostic Lung Cancer 1 4 Recruiting Other Type 1 Diabetes Mellitus 1 4 Terminated Basic Science Abdominal Aortic Aneurysm (AAA) 1 4 Terminated Treatment Asthma 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Parenteral 185 MBq/ml Injection, solution Parenteral 1500 MBq/ml Injection, solution Parenteral 2200 MBq/ml Injection, solution Parenteral 3100 MBq/ml Injection Intravenous Injection, solution Parenteral 1 GBq/ml Injection, solution Parenteral 7.6125 GBq Injection, solution Intravenous Injection Intravenous 0.5 Ci/1mL Injection Intravenous 20 mCi/1mL Injection Intravenous 240 mCi/1mL Injection Intravenous 40 mCi/1mL Injection, solution Intravenous 100 mCi/1mL Injection, solution Intravenous 300 mCi/1mL Injection, solution Intravenous 475 mCi/1mL Injection Intravenous 200 mCi/1mL Injection Intravenous 500 mCi/1mL Injection, solution Intravenous 200 mCi/1mL Injection, solution Intravenous 500 mCi/1mL Injection Intravenous 12.5 mCi/ml Injection Intravenous 100 mCi/1mL Injection Intravenous 300 mCi/1mL Injection Intravenous 400 mCi/1mL Injection, solution Intravenous 0.3 Ci/1mL Injection, solution Intravenous; Parenteral 185 MBq/ml Injection, solution Injection, solution Intravenous; Parenteral 250 MBq/ml Injection, solution Intravenous; Parenteral 600 MBq/ml Solution Intravenous 1650 MBq Solution Intravenous 250 MBq/ml Injection, solution 250 MBq/ml Injection, solution Intravenous; Parenteral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 139.0 mg/mL ALOGPS logP -1.8 ALOGPS logP -2.7 Chemaxon logS -0.12 ALOGPS pKa (Strongest Acidic) 10.32 Chemaxon pKa (Strongest Basic) -3 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 97.99 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 35.65 m3·mol-1 Chemaxon Polarizability 15.54 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-03kc-9400000000-654e7384b2d5ad26d4c0 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-00ke-4900000000-4cddcdd49492d9027c21 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-9000000000-ba86c875a092d5c8a5a8 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03dl-9100000000-a93285cc5c6ddf3a10df Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0avi-9000000000-97a70bb577ce5cdd1f31 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0005-9000000000-c46b9f8769e60147d76d Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-052f-9000000000-7b16fed320d58c285cef Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Mannokinase activity
- Specific Function
- Not Available
- Gene Name
- HK1
- Uniprot ID
- P19367
- Uniprot Name
- Hexokinase-1
- Molecular Weight
- 102485.1 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucose transmembrane transporter activity
- Specific Function
- Insulin-regulated facilitative glucose transporter.
- Gene Name
- SLC2A4
- Uniprot ID
- P14672
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 4
- Molecular Weight
- 54786.79 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Hexose transmembrane transporter activity
- Specific Function
- Facilitative glucose transporter. This isoform likely mediates the bidirectional transfer of glucose across the plasma membrane of hepatocytes and is responsible for uptake of glucose by the beta c...
- Gene Name
- SLC2A2
- Uniprot ID
- P11168
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 2
- Molecular Weight
- 57488.955 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic transporter activity
- Specific Function
- Facilitative glucose transporter. This isoform may be responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including b...
- Gene Name
- SLC2A1
- Uniprot ID
- P11166
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 1
- Molecular Weight
- 54083.325 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucose transmembrane transporter activity
- Specific Function
- Facilitative glucose transporter that can also mediate the uptake of various other monosaccharides across the cell membrane (PubMed:9477959, PubMed:26176916). Mediates the uptake of glucose, 2-deox...
- Gene Name
- SLC2A3
- Uniprot ID
- P11169
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 3
- Molecular Weight
- 53923.785 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sugar:proton symporter activity
- Specific Function
- Transport urate and fructose. May have a role in the urate reabsorption by proximal tubules. Also transports glucose at low rate.
- Gene Name
- SLC2A9
- Uniprot ID
- Q9NRM0
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 9
- Molecular Weight
- 58701.205 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucose transmembrane transporter activity
- Specific Function
- Cytochalasin B-sensitive carrier. Seems to function primarily as a fructose transporter.
- Gene Name
- SLC2A5
- Uniprot ID
- P22732
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 5
- Molecular Weight
- 54973.42 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucose transmembrane transporter activity
- Specific Function
- Facilitative glucose transporter; binds cytochalasin B with low affinity.
- Gene Name
- SLC2A6
- Uniprot ID
- Q9UGQ3
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 6
- Molecular Weight
- 54538.55 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Substrate-specific transmembrane transporter activity
- Specific Function
- High-affinity transporter for glucose and fructose Does not transport galactose, 2-deoxy-d-glucose and xylose.
- Gene Name
- SLC2A7
- Uniprot ID
- Q6PXP3
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 7
- Molecular Weight
- 55726.915 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Glucose transmembrane transporter activity
- Specific Function
- Insulin-regulated facilitative glucose transporter. Binds cytochalasin B in a glucose-inhibitable manner. Seems to be a dual-specific sugar transporter as it is inhibitable by fructose (By similari...
- Gene Name
- SLC2A8
- Uniprot ID
- Q9NY64
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 8
- Molecular Weight
- 50818.54 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Sugar:proton symporter activity
- Specific Function
- Facilitative glucose transporter.
- Gene Name
- SLC2A10
- Uniprot ID
- O95528
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 10
- Molecular Weight
- 56910.77 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Substrate-specific transmembrane transporter activity
- Specific Function
- Facilitative glucose transporter.
- Gene Name
- SLC2A11
- Uniprot ID
- Q9BYW1
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 11
- Molecular Weight
- 53702.055 Da
References
- FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Substrate-specific transmembrane transporter activity
- Specific Function
- Facilitative glucose transporter.
- Gene Name
- SLC2A12
- Uniprot ID
- Q8TD20
- Uniprot Name
- Solute carrier family 2, facilitated glucose transporter member 12
- Molecular Weight
- 66965.7 Da
References
- FDA Label [Link]
Drug created at November 30, 2015 19:10 / Updated at December 04, 2021 06:47